Bioactive moieties designed to bind to cell membrane receptors benefit from coupling with polymeric carriers that have enhanced affinity to the cell membrane. When bound to the cell surface, such carriers create a "2D solution" of a ligand with a significantly increased concentration near a membrane-bound receptor compared to a freely water-soluble ligand. Bifunctional polymeric carriers based on amphiphilic triblock copolymers were synthesized from 2-pent-4-ynyl oxazoline, 2-nonyl oxazoline and 2-ethyl oxazoline. Their self-assembly and interactions with plasma proteins and HEK 293 cells were studied in detail. The affinity of these triblock copolymers to HEK 293 cell membranes and organ tissues was tunable by the overall hydrophobicity of the polymer molecule, which is determined by the length of the hydrophobic and hydrophilic blocks. The circulation time and biodistribution of three representative triblock copolymers were monitored after intravenous administration to C57BL/6 albino mice. A prolonged circulation time was observed for polymers with longer hydrophobic blocks, despite their molecular weight being below the renal threshold.
- Klíčová slova
- Amphiphilic triblock polyoxazoline, Biodistribution in vivo, Blood proteins, Drug delivery, HEK 293 cells, Isothermal titration calorimetry,
- MeSH
- buněčná membrána MeSH
- cytoplazma MeSH
- HEK293 buňky MeSH
- hydrofobní a hydrofilní interakce MeSH
- lidé MeSH
- ligandy MeSH
- micely * MeSH
- myši MeSH
- polymery * chemie MeSH
- tkáňová distribuce MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- ligandy MeSH
- micely * MeSH
- poly(2-oxazoline) MeSH Prohlížeč
- polymery * MeSH
